| Identification | Back Directory | [Name]
TYRPHOSTIN B7 | [CAS]
134036-53-6 | [Synonyms]
AG 370
TYRPHOSTIN B7
TYRPHOSTIN AG 370
TYROPHOSTIN AG 370
2-AMINO-4-(1H-INDO-5'-YL)-1,1,3-TRICYANOBUTA-1,3-DIENE
2-AMINO-4-(1H-INDOL-5-YL)-1,1,3-TRICYANOBUTA-1,3-DIENE
3-AMINO-4-(1H-INDOL-5-YLMETHYLENE)-2-PENTENETRICARBONITRILE
2-Pentenetricarbonitrile, 3-amino-4-(1H-indol-5-ylmethylene)-
2-Amino-4-(1H-indo-5μ-yl)-1,1,3-tricyanobuta-1,3-diene, Tyrphostin B7 | [Molecular Formula]
C15H9N5 | [MDL Number]
MFCD00236449 | [MOL File]
134036-53-6.mol | [Molecular Weight]
259.27 |
| Chemical Properties | Back Directory | [Boiling point ]
714.1±60.0 °C(Predicted) | [density ]
1.396±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C | [solubility ]
DMSO: soluble | [form ]
Yellow solid. | [pka]
15.95±0.30(Predicted) |
| Hazard Information | Back Directory | [Description]
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues. AG-370 is a selective inhibitor of PDGF receptor kinase with an IC50 value of 20 μM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC50 = 820 μM). | [Definition]
ChEBI: AG-370 is a member of indoles. | [in vitro]
previous study found that ag-370 inhibited pdgf receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates that coprecipitated with the pdgf receptor in digitonin-permeabilized fibroblasts and in intact fibroblasts. when compared with ag18, a potent egf receptor blocker, ag370 was more efficient in inhibiting pdgf-induced proliferation of fibroblasts and phosphorylation of the intracellular protein substrates. under the conditions in which ag370 could inhibit pdgf-induced mitogenesis and phosphorylation, ag18 did not alter [125i]pdgf internalization and enhance [125i]pdgf binding. these findings suggested that ag370 might have a therapeutic potential for treatment of diseases involving abnormal cellular proliferation induced by pdgf [1]. | [IC 50]
20 μm for pdgf receptor kinase in human bone marrow fibroblasts | [storage]
Store at -20°C | [References]
[1] bryckaert, m. c.,eldor, a.,fontenay, m., et al. inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. experimental cell research 199, 255-261 (1992). |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
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| Tel: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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